The tetrapeptide Arg-Gly-Asp-Ser (RGDS) is a key component of the cell attachment domain of fibronectin. The RGDS sequence was found initially to promote the attachment of rat kidney fibroblasts (NRKcells) to fibronectin and synthetic fibronectin peptides coupled to protein-coated plastic. Further investigation indicated that the free RGDS peptide inhibited the attachment of NRK cells to fibronectin coated substrates. The RGDS sequence has been shown to occur in several other proteins, such as the λ receptor on E. coli and the Sindbis coat protein. RGDS is also a target sequence for spirochete adherence of the syphilis bacterium Treponema pallidum.
RGDS has been shown to block fibrinogen-induced aggregation of intact erythrocytes and specific binding of fibrinogen to erythrocyte membranes. The effect of RGDS on transforming growth factor ?1 (TGF?1) mRNA expression and secretion in cultured human mesangial cells has been investigated. RGDS has been utilized in a study of integrin-mediated signal transduction in cultured cells from the sponge Suberites domuncula. RGDS has been demonstrated
to mitigate the binding of Mycobacterium tuberculosis to murine alveolar macrophages
rgds peptide contains the rgd motif which is an antagonist of integrin [1, 2].integrins are cell-surface receptors that recognize rgd motifs present in various extracellular matrix proteins such as fibronectin, vitronectin, laminin, fibrinogen, von willebrand factor, osteopontin, thrombospondin, and collagen as well as in disintegrins. integrins activation triggers different signals regulating cell adhesion, migration, survival, apoptosis as well as processes such as angiogenesis, thrombosis and osteoporosis [1].in sk-mel-110 cells, rgds at 500 μg/ml significantly inhibited melanoma cells proliferation induced by human fibroblast growth factor-2 (fgf-2). furthermore, rgds treatment (48 h, 500 μg/ml) increased the percentage of cells in sub-g1-phase from 3% (with fgf-2 alone) to 13.2% (with fgf-2 and rgds), indicating that rgds might induce apoptosis in melanoma cells, in the presence of fgf-2 [1].in a guinea pig model of allergic asthma, topical treatment of the airways with intranasally instilled rgds (2.5 mm, 200 μl) attenuated allergen-induced airway smooth muscle hyperplasia and hypercontractility as well as increased pulmonary expression of smooth muscle myosin heavy chain and the proliferative marker proliferating cell nuclear antigen [2].[1]. aguzzi m s, fortugno p, giampietri c, et al. intracellular targets of rgds peptide in melanoma cells. molecular cancer, 2010, 9(84): 1-10.[2]. dekkers b g, bos i s, gosens r, et al. the integrin-blocking peptide rgds inhibits airway smooth muscle remodeling in a guinea pig model of allergic asthma. american journal of respiratory and critical care medicine, 2010, 181(6): 556-565.
